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Assay Detail

CHEMBL616120

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of specific [3H]- 5-HT binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Parallel synthesis of 3-aryloxy-2-propanolamines and evaluation as dual affinity 5-HT(1A) and 5-HT re-uptake ligands.
van Niel MB, Beer MS, Castro JL, Cheng SK, Evans DC, Heald A, Hitzel L, Hunt P, Mortishire-Smith R, O'Connor D, Watt AP, MacLeod AM.
Bioorg Med Chem Lett (1999) 9 : 3243 -3248
PubMed 10576696 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.35 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL327126 1 9.00
CHEMBL326751 1 8.96
CHEMBL111065 1 8.77
CHEMBL114452 1 8.66
CHEMBL111713 1 8.64
CHEMBL111021 1 8.55
CHEMBL112841 1 8.26
CHEMBL323441 1 8.22
CHEMBL114453 1 8.08
CHEMBL500 PINDOLOL 4.0 1 7.62
CHEMBL113326 1 7.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL327126 Ki = 1.0 nM 9.00
CHEMBL326751 Ki = 1.1 nM 8.96
CHEMBL111065 Ki = 1.7 nM 8.77
CHEMBL114452 Ki = 2.2 nM 8.66
CHEMBL111713 Ki = 2.3 nM 8.64
CHEMBL111021 Ki = 2.8 nM 8.55
CHEMBL112841 Ki = 5.5 nM 8.26
CHEMBL323441 Ki = 6.0 nM 8.22
CHEMBL114453 Ki = 8.3 nM 8.08
CHEMBL500 PINDOLOL Ki = 24.0 nM 7.62
CHEMBL113326 Ki = 72.0 nM 7.14